• Computational approaches such as docking and classical molec

  2021-11-30

  

  Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over

• br Results br Discussion br STAR Methods br Acknowledgments

  2021-11-30

  

  Results Discussion STAR★Methods Acknowledgments The authors thank Drs. Michael Wegner, Ron Waclaw, and Ed Hurlock for critical comments. We thank Drs. Lihui Tsai and Jiang Wu for CHD8 and ASH2L-expressing vectors, respectively, Dr. Yueh-Chiang Hu for generating transgenic lines, and Jing

• The medicinal properties of guanidine derivatives are also o

  2021-11-30

  

  The medicinal properties of guanidine derivatives are also of great interest due to their diverse anti-microbial, anti-inflammatory, anti-viral, and anti-cancer, activities (C and D). Guanidine-containing drugs, such as -iodobenzylguanidine and methylglyoxal bis(guanylhydrazone), were shown several

• Nazar and colleagues reported a

  2021-11-30

  

  Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been

• br Results and discussion br Conclusions A series

  2021-11-30

  

  Results and discussion Conclusions A series of novel HDAC inhibitors comprising the thioquinazolinone were designed and synthesized. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines. Then we chose compounds 7a, 4i, 4o, and 4p to fu

• br General aspects of HDACs br General aspects of HDAC

  2021-11-30

  

  General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai

• Nilvadipine For the SAR study human haspin kinase inhibitory

  2021-11-30

  

  For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat

• We have shown previously that activation of the

  2021-11-30

  

  We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates 3-Chlorotyrosine cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic TGFβ-induce

• Cells undergoing EMT display a

  2021-11-30

  

  Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the HOAt cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junctions are specialized cell-ce

• 10-Hydroxycamptothecin receptor The HIV genome encodes for

  2021-11-29

  

  The HIV-1 genome encodes for a variety of viral proteins necessary for target cell entry and viral replication. gp120 is an HIV-1 envelope glycoprotein that mediates viral particle entry by binding to cell surface receptor CD4 and co-receptors CXCR4 and/or CCR5 depending on viral tropism. While CXCR

• Up to now many UDG assays have been reported

  2021-11-29

  

  Up to now, many UDG assays have been reported based on the design of dU-containing substrate DNA, which can be roughly divided into two categories according to the sensing mechanisms. One type of UDG assays are simply based on the physical or chemical property changes of the substrate accompanied wi

• Through the analysis of various

  2021-11-29

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Sometimes motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TA

• Although EAAT may not be involved in the

  2021-11-29

  

  Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few

• br Introduction The glucagon receptor GCGR is

  2021-11-29

  

  Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m

• Another consistent observation in our studies was the

  2021-11-29

  

  Another consistent observation in our studies was the lower plasma catecholamine concentrations in the exercised GHSR-null mice, suggesting a diminished sympathoadrenal response. A proper sympathoadrenal response is essential for increasing substrate utilization during exercise [81]. Thus, the reduc

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